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Halogenated benzimidazoles and benzotriazoles as inhibitors of the NTPase/helicase activities of hepatitis C and related viruses.
- P. Borowski, Johanna Deinert, +4 authors D. Shugar
- Biology, Medicine
- European journal of biochemistry
- 1 April 2003
A search has been initiated for lead inhibitors of the nonstructural protein 3 (NS3)-associated NTPase/helicase activities of hepatitis C virus, the related West Nile virus, Japanese encephalitis… Expand
Purification and Characterization of West Nile Virus Nucleoside Triphosphatase (NTPase)/Helicase: Evidence for Dissociation of the NTPase and Helicase Activities of the Enzyme
ABSTRACT The nucleoside triphosphatase (NTPase)/helicase associated with nonstructural protein 3 of West Nile (WN) virus was purified from cell culture medium harvested from virus-infected Vero… Expand
Inhibition of the helicase activity of HCV NTPase/helicase by 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide-5 '-triphosphate (ribavirin-TP).
In the presented study the ribavirin-TP--an established inhibitor of the NTPase activity of the superfamily NTPase/helicases II--was investigated as an inhibitor of the unwinding activity of the… Expand
2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity.
- M. Bretner, T. Kulikowski, J. Dzik, M. Balińska, W. Rode, D. Shugar
- Chemistry, Medicine
- Journal of medicinal chemistry
- 12 November 1993
A convenient synthesis of 5-fluoro-2-thiouracil (11) is based on hydrolytic deamination of 5-fluoro-2-thiocytosine (9). Lewis acid-catalyzed condensation of di-TMS-5-fluoro-2-thiouracil (13) or… Expand
Modified 5′‐Trityl Nucleosides as Inhibitors of Plasmodium falciparum dUTPase
2′‐Deoxyuridine triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for the treatment of malaria. We previously reported the discovery of 5′‐tritylated analogues of deoxyuridine as… Expand
High-Yield Regioselective Thiation of Biologically Important Pyrimidinones, Dihydropyrimidinones and Their Ribo, 2′-Deoxyribo and 2′, 3′-Dideoxyribo Nucleosides
Abstract Convenient and high-yield regioselective thiation procedures based on the use of the Lawesson reagent in different solvents, are described for conversion of the 2- and 4-keto, and 2,… Expand
Studies on the interaction with thymidylate synthase of analogues of 2'-deoxyuridine-5'-phosphate and 5-fluoro-2'-deoxyuridine-5'-phosphate with modified phosphate groups.
- W. Rode, T. Kulikowski, B. Kedzierska, D. Shugar
- Chemistry, Medicine
- Biochemical pharmacology
- 15 January 1987
The role of the phosphate moiety of dUMP, and some analogues, in their interaction with mammalian thymidylate synthase, has been investigated. Substrate and inhibitor activities, and the… Expand
Interaction of 2-thio-5-fluoro-dUMP and 4-thio-5-fluoro-dUMP with mammalian normal and tumour and helminthic thymidylate synthases: influence of C(4)-substituents on specificity for enzyme…
- J. Dzik, Z. Zieliński, +5 authors W. Rode
- Biology, Medicine
- Biochemical and biophysical research…
- 30 September 1993
To determine how 5-fluoro-dUMP modifications may affect its specificity, 2-thio-5-fluoro-dUMP and 4-thio-5-fluoro-dUMP were compared as inhibitors of thymidylate synthases isolated from parental and… Expand
Trichinella spiralis and Trichinella pseudospiralis: developmental patterns of enzymes involved in thymidylate biosynthesis and pyrimidine salvage.
Thymidylate synthase, dihydrofolate reductase and dUTPase specific activities were found to remain at a high and constant level in crude extracts from adult worms of Trichinella spiralis, as well as… Expand
Partial selective inhibition of HIV-1 reverse transcriptase and human DNA polymerases γ and β by thiated 3'-fluorothymidine analogue 5'-triphosphates.
3'-Deoxy-3'-fluorothymidine (FLT, alovudine(®)) belongs to the most potent agents inhibiting HIV-1 replication. Its 5'-triphosphate (FLTTP) is a potent inhibitor of HIV-1 reverse transcriptase (HIV… Expand